Activators & Inhibitors

PP242 is an inhibitor at the kinase domain of the mammalian target of rapamycin (mTOR), which is a Ser/Thr kinase and a cell growth controller. PP242 inhibits mTORC1 more effectively than rapamycin. Unlike rapamycin, PP242 inhibits both mTORC1 and mTORC2 with IC50 values of 0.03 and 0.058 µM, respectively and it can inhibit cap-dependent translation. PP242 functions by blocking the phosphorylation of Akt at S473 and preventing mTOR activation. PP242 exhitibits IC50 values for other kinases of 0.11 µM (JAK2), 0.41 µM (DNAPK), 0.05 µM (PKC?), 0.2 µM (PKCβ I and II), 4.4 µM (EGFR), and1.5 µM (VEGFR2).

Axitinib (AG-013736) is an oral, potent, and selective inhibitor of vascular endothelial growth factor receptors 1 (VEGFR-1), 2 (VEGFR-2), and 3 (VEGFR-3), platelet derived growth factor receptor (PDGFR), and cKIT (CD117).

Forskolin is a cell permeable adenylate cyclase activator which causes an increase in the intracellular concentration of cAMP. This makes it an important hypotensive and vasodilatory agent. Forskolin also affects calcium currents and inhibits PKC (Protein Kinase C)-stimulated MAPK and RAF-1.

Forskolin is a cell permeable adenylate cyclase activator which causes an increase in the intracellular concentration of cAMP. This makes it an important hypotensive and vasodilatory agent. Forskolin also affects calcium currents and inhibits PKC (Protein Kinase C)-stimulated MAPK and RAF-1.

XAV 939 is a small molecule and selective Wnt pathway transcription factor - catenin-mediated transcription inhibitor and axin stabilizing agent. It stimulates beta-catenin degradation by stabilizing axin, the concentration-limiting component of the destruction complex and stabilizes axin by inhibiting the poly-ADP-ribosylating enzymes tankyrase 1 (TNKS1) and tankyrase 2 (TNKS2).

ABT-888 (Veliparib) is a potent inhibitor of both PARP-1 and PARP-2. In the MX-1 breast xenograft model (BRCA1 deletion and BRCA2 mutation), ABT-888 potentiated cisplatin, carboplatin, and cyclophosphamide, causing regression of established tumors, whereas with comparable doses of cytotoxic agents alone, only modest tumor inhibition was exhibited.

Trichostatin A (TSA) is an antifungal antibiotic with cytostatic and differentiating properties in mammalian cell culture.

EX 527 is a potent and selective SIRT1 class III histone deacetylase enzyme inhibitor. It is Selective inhibitor of SIRT1 that does not class I/II inhibit histone deacetylase (HDAC) or other sirtuin deacetylase family members. EX 527 has been used a powerful tool for studying the relationship between SIRT1 and cell regulation.

Curcumin, also known as diferuloylmethane, natural yellow 3, or C.I. 75300, is the principal curcuminoid of the popular Indian spice turmeric, which is a small molecule, selective HAT inhibitor. It has shown to promote degradation of p300 and inhibits the acetyltransferases activity of purified p300 using either histone H3 or p53 as a substrate.